1508250-71-2 Usage
Description
EGF816, also known as Nazartinib, is an irreversible inhibitor of mutant epidermal growth factor receptors (EGFRs). It is specifically designed to target EGFR mutant cell lines, demonstrating high selectivity and potency against various lung adenocarcinoma and non-small cell lung cancer cells. EGF816 effectively decreases the phosphorylation of EGFR, leading to the inhibition of cell proliferation in these cancerous cells.
Uses
Used in Oncology:
EGF816 is used as an anticancer agent for the treatment of lung adenocarcinoma and non-small cell lung cancer (NSCLC). It selectively targets EGFR mutant cell lines, such as H3255, HCC827, and H1975, with high potency and minimal impact on cells expressing wild-type EGFRs. EGF816 has been shown to reduce tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.
Used in Drug Development:
EGF816 is used as a research tool in the development of targeted therapies for EGFR mutant cancers. Its high selectivity and potency make it a valuable compound for studying the mechanisms of action and potential therapeutic applications in oncology research.
Used in Pharmaceutical Industry:
EGF816 is used as a starting point for the development of new drugs targeting EGFR mutant cancers. Its unique properties and effectiveness against specific cancer cell lines make it a promising candidate for further optimization and development into a therapeutic agent for lung adenocarcinoma and NSCLC patients.
in vitro
egf816 showed sustained inhibition of pegfr, which is consistent with the irreversible binding mechanism of egf816. egf816 also performs exceptionally well in long term dosing studies providing durable responses in the preclinical models [1].
in vivo
egf816 demonstrated strong in vivo tumor regressions in several egfr activating and resistant tumor models. in all of the models egf816 inhibited tumor growth dose-dependently and achieved regressions of established tumors at well tolerated doses [1].
references
[1] shailaja kasibhatla, jie li, celin tompkins, mei-ting vaillancourt, jennifer anderson, annemarie culazzo pferdekamper, chun li, oliver long, mathew mcneill, robert epple, debbie liao, eric murphy, steve bender, yong jia, gerald lelais. egf816, a novel covalent inhibitor of mutant-selective epidermal growth factor receptor, overcomes t790m-mediated resistance in nsclc. [abstract]. in: proceedings of the 105th annual meeting of the american association for cancer research; 2014 apr 5-9; san diego, ca. philadelphia (pa): aacr; cancer res 2014;74(19 suppl):abstract nr 1733. doi:10.1158/1538-7445.am2014-1733
Check Digit Verification of cas no
The CAS Registry Mumber 1508250-71-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,0,8,2,5 and 0 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1508250-71:
(9*1)+(8*5)+(7*0)+(6*8)+(5*2)+(4*5)+(3*0)+(2*7)+(1*1)=142
142 % 10 = 2
So 1508250-71-2 is a valid CAS Registry Number.
